Clinical Pharmacokinetics of Articaine

Abstract

Articaine is the most widely used local anaesthetic agent in dentistry in a number of European countries. The amide structure of articaine is similar to that of other local anaesthetics, but it contains an additional ester group which is quickly hydrolysed by esterases. High performance liquid chromatography has been used to determine the concentrations of articaine and its metabolite articainic acid in serum. Rapid sample preparation is critical in the accurate determination of articaine serum concentrations, since blood and serum are the sites of metabolism. The time to maximum drug concentrations of articaine occurs about 10 to 15 minutes after submucosal injection of articaine 4% 80 mg, irrespective of epinephrine (adrenaline). The mean maximum plasma drug concentration is about 400 micrograms/L for articaine with epinephrine 1:200,000 and 580 micrograms/L for articaine without epinephrine. The elimination half-time of articaine is about 20 minutes. The rapid breakdown of articaine to the inactive metabolite articainic acid is related to a very low systemic toxicity and consequently to the possibility of repeated injections. Equal analgesic efficacy along with lower systemic toxicity (i.e. a wide therapeutic range) permits the use of articaine in higher concentrations than other amide-type local anaesthetics. Complete anaesthesia can be observed in nearly 90% of all cases, using articaine 4% 60 to 80 mg with epinephrine 1:200,000. Articaine is better able to diffuse through soft tissue and bone than other local anaesthetics. The concentration of articaine in the alveolus of a tooth in the upper jaw after extraction was about 100 times higher than that in systemic circulation. The plasma protein binding rate of articaine and articainic acid is 70%. It has been concluded that an unintentional intravascular injection of articaine 80 mg does not cause toxic effects in healthy individuals.

Extraction of Permanent Maxillary Teeth by Only Buccal Infiltration of Articaine

“…Hence it can be stated that palatal anesthesia achieved by depositing articaine to the buccal vestibule was as effective as palatal infiltration of lignocaine. This finding is in accordance with the study done by Sina et al [1], Oertel et al [6], Grace et al [7] and Song et al [8].…”

Ropivacaína, articaína ou combinação de ropivacaína e articaína em anestesia peridural para cesariana: estudo randomizado, prospectivo e duplo-cego

“…This structural characteristic increases the lipid solubility of articaine and speeds its onset of action 14,15 . In addition, we know that the pH and pKa of local anesthetics affect their onset of action.…”

“…However, ropivacaine provides a similar speed of sensory block onset as bupivacaine but does not provide faster onset for epidural anesthesia [11][12][13] . An amide group local anesthetic, articaine, has a fast onset and offset time due to its high lipid solubility 14,15 . Articaine has a short sensory and motor block onset of action and low toxicity profi le; its use had been described for epidural anesthesia [15][16][17][18] .…”

“…An amide group local anesthetic, articaine, has a fast onset and offset time due to its high lipid solubility 14,15 . Articaine has a short sensory and motor block onset of action and low toxicity profi le; its use had been described for epidural anesthesia [15][16][17][18] . The use of combinations of different local anesthetics for epidural anesthesia in cesarean surgeries has been studied in the literature 9,10 , however we did not come across any study that combines articaine and ropivacaine for epidural anesthesia.…”

Efeitos cardiovasculares da infiltração maxilar da articaína e lidocaína associadas à epinefrina em procedimentos restauradores

“…A articaína difere dos demais anestésicos do tipo amida por duas características que lhe são peculiares: primeiro, o fato de possuir um anel tiofeno ao invés de um anel benzeno em sua porção lipofílica, o que seria responsável por conferir-lhe maior lipossolubilidade em relação aos demais anestésicos (LEMAY et al, 1984;OERTEL;RAHN;KIRCH, 1997), e, segundo, por possuir uma cadeia radical éster, que permite sua biotransformação no plasma através da ação das plasma esterases, bem como no fígado, pelas enzimas microssomais hepáticas, isso provocaria uma hidrólise relativamente mais rápida, que ajudaria a diminuir a toxicidade associada à redução lenta da droga do local de injeção (YAGIELA, 1998).…”